GW7647

别名

GW7647 - CAS 265129-71-3 - Calbiochem,GW647, 2-(4-(2-(1-Cyclohexanebutyl-3-cyclohexylureido)ethyl)phenylthio)-2-methylpropionic Acid, PPAR Agonist IV, PPARα Agonist II, PPARβ/δ Agonist I, PPARγ Agonist III

一般描述

A cell-permeable urea-substituted thioisobutyric acid (ureido-TiBA) compound that acts as a potent and selective PPARα agonist (PPARα, γ and δ - EC50 = 6 nM, 1.1 µM and 6.2 µM for human; 1 nM, 1.3 µM and 2.9 µM for murine, respectively). Also displays in vivo lipid-lowering activity in rats. A cell-permeable, urea-substituted, thioisobutyric acid (ureido-TiBA) compound that acts as a potent and selective peroxisome proliferator-activated receptor α (PPARα) agonist (EC50 = 6 nM for human PPARα, 1.1 µM for human PPARγ, and 6.2 µM human PPARδ; 1 nM for murine PPARα, 1.3 µM for murine PPARγ, and 2.9 µM murine PPARδ). Also shown to lower lipid levels in rats.

生化/生理作用

Cell permeable: yes EC50 = 6 nM, 1.1 µM and 6.2 µM for human PPARα, γ and δ, respectively; EC50 = 1 nM, 1.3 µM and 2.9 µM for murine PPARα, γ and δ, respectively Primary Target
PPARα Product does not compete with ATP. Reversible: no

其他说明

Muoio, D.M., et al. 2002. J. Biol. Chem.277, 26089.
Brown, P.J., et al. 2001. Bioorg. Med. Chem. Lett.11, 1225.
Oliver, W.R. Jr., et al. 2001. Proc. Natl. Acad. Sci. USA98, 5306.
Poirier, H., et al. 2001. Biochem. J.355, 481.